📜3-Benzoylamino-Benzoic Acid Methyl Ester置于水,Sodium Hydroxide体系中,用 甲醇 作为反应溶剂,化学反应 2.0H,反应生成 5,7-二甲基吡唑并嘧啶-2-羧酸
参考文献:Structure-Based Design And Synthesis Of Novel Inhibitors Targeting Hdac8 From Schistosoma Mansoni For The Treatment Of Schistosomiasis
标题:Structure-Based Design And Synthesis Of Novel Inhibitors Targeting Hdac8 From Schistosoma Mansoni For The Treatment Of Schistosomiasis
摘要:Schistosomiasis Is A Major Neglected Parasitic Disease That Affects More Than 265 Million People Worldwide And For Which The Control Strategy Consists Of Mass Treatment With The Only Available Drug,Praziquantel. In This Study,A Series Of New Benzohydroxamates Were Prepared As Potent Inhibitors Of Schistosoma Mansoni Histone Deacetylase 8 (Smhdac8). Crystallographic Analysis Provided Insights Into The: Inhibition Mode Of Smhdac8 Activity By These 3-Amidobenzohydroxamates. The Newly Designed Inhibitors Were Evaluated In Screens For Enzyme Inhibitory Activity Against Schistosome And Human Hdacs. Twenty-Seven Compounds Were Found To Be Active In The Nanomolar Range,And Some Of Them Showed Selectivity Toward Smhdac8 Over The Major Human Hdacs (I And 6). The Active Benzohydroxamates Were Additionally Screened For Lethality Against The Schistosome Larval Stage Using A Fluorescence-Based Assay. Four Of These Showed Significant Dose-Dependent Killing Of The Schistosome Larvae And Markedly Impaired Egg Laying Of Adult Worm Pairs Maintained In Culture.
DOI:10.1021/acs.Jmedchem.5B01478